An orally bioavailable Bcl-xL inhibitor; selectively binds Bcl-xL over Bcl-2

A-1331852 – 1 mg

Brand:
Cayman
CAS:
1430844-80-6
Storage:
-20
UN-No:
Non-Hazardous - /

A-1331852 is an orally bioavailable Bcl-xL inhibitor that selectively binds Bcl-xL over Bcl-2, Mcl-1, and Bcl-W (Kis = in vitro (EC50s = 6 and >5,000 nM, respectively). A-1331852 (25 mg/kg twice per day) inhibits tumor growth in a MOLT-4 mouse xenograft model. It also inhibits tumor growth and increases the antitumor activity of docetaxel (Item No. 11637) in MDA-MB-231 LC3 metastatic breast cancer and NCI-H1650 non-small cell lung cancer mouse xenograft models when administered at a dose of 25 mg/kg. A-1331852 also increases venetoclax inhibition of tumor growth in an NCI-H1963.FP5 small cell lung cancer mouse xenograft model.  

 

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SKU: 22963 - 1 mg Category:

Description

An orally bioavailable Bcl-xL inhibitor; selectively binds Bcl-xL over Bcl-2, Mcl-1, and Bcl-W (Kis = in vitro (EC50s = 6 and >5,000 nM, respectively); inhibits tumor growth in a MOLT-4 mouse xenograft model at 25 mg/kg; inhibits tumor growth and increases the antitumor activity of docetaxel in MDA-MB-231 LC3 metastatic breast cancer and NCI-H1650 non-small cell lung cancer mouse xenograft models at 25 mg/kg

Formal name: 6-[8-[(2-benzothiazolylamino)carbonyl]-3,4-dihydro-2(1H)-isoquinolinyl]-3-[5-methyl-1-(tricyclo[3.3.1.13,7]dec-1-ylmethyl)-1H-pyrazol-4-yl]-2-pyridinecarboxylic acid

Synonyms: 

Molecular weight: 658.8

CAS: 1430844-80-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Migration & Metastasis

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